2010 尖吻蝮蛇血凝酶药效评价及其作用机制.pdf

Chinese Journal ofN ew Drugs 2010, 19( 18) , , , , , , (南方医科大学药学院, 广州 510515) [] : 研究注射用尖吻蝮蛇血凝酶(HaemocoagulaseAgkistrodon, HCA, 商品名苏灵)的止血效果 其作用机制: 通过体内外形成血栓实验, 了解药物的凝血效果 其是否激活凝血因子 !; 通过HCA 对 纤维蛋白原的裂解作用探讨其凝血机制: HCA作用下体内外形成血栓的大小与立止血相差不大, 差异无 统计学意义; 蛋白凝胶电泳图显示HCA 作用 12 h后纤维蛋白原 亚基带消失; 高效液相色谱图显示在 8. 8m in 处有明显的峰出现: HCA 具有良好的止血效果,且不激活凝血因子 !; HCA 能水解纤维蛋白原的 亚 基, 裂解出A 肽片段( FpA), 形成纤维蛋白单体( B ) , 并聚合成纤维蛋白多聚体, 发挥止血作用 2 [] 尖吻蝮蛇血凝酶; 止血机制; 药效评价; 纤维蛋白原; 凝血因子 ! [] R9 3. 2 [] A [] 1003- 3 34( 2010) 18- 1 06- 04 Evaluation of hemostatic effectsofH aem ocoagulase Agk istrodon and themechanisms SH IGuang, PANG Jianxin, KONG Huanyu, LUO Chao, LIU A im ing, JIN Hong, CAO Y ing (School of PharmaceuticalSciences, SouthernM edical University, Guangzhou 510515, China) [Abstract] Objective: To evaluate the hemostatic effect ofH aemocoagulase Agkistrodon ( HCA, trade name: Su ling) for injection and the mechan isms. M ethods: In the in vivo and in vitro expermi ents of thrombosis, the hemostatic effects ofHCA and activation of coagulation factor ! in blood coagu lation w ere evaluated. The mechan ismsw ere investigated by determ in ing the ab ility of HCA to degrade fibrinogen. Results: HCA had the effect smi ilar to the positive control reptilase, but the d ifferencew as not statistically significant. SDSpolyacrylam ide gel electrophoresis show ed that the chain d isappeared after 12 h incubationw ith HCA, and h igh performance liq u id chrom atography show ed an obvious peak at 8. 8m in. Conclusion: HCA has a good hemostatic effect w ithout activating coagulation factor !. It exerts hemostatic effect by hydrolyzing chain of fibrinogen, releasingA pep tide fragment ( FpA ) to generate the fibrin monomers ( B ) and polymerizin